Evaluation of 4-alkoxychalcones as a new class of antiglycating agents: a combined experimental and docking study

Evaluation of 4-alkoxychalcones as a new class of antiglycating agents: a combined experimental...
Abbas, Asghar; Kalsoom, Saima; Hadda, Taibi; Naseer, Muhammad
2014-07-10 00:00:00
A series of 4-alkoxychalcones (1–12) has been evaluated for their in vitro antiglycation activity. Compound 2 (IC50 = 89.07 ± 1.3 μM), compound 3 (IC50 = 266.82 ± 4.6 μM), and compound 5 (IC50 = 285.79 ± 1.9 μM) showed an excellent antiglycation potential better than the standard (rutin, IC50 = 294.50 ± 1.5 μM). Additionally, all the compounds of this series were evaluated for their cytotoxicity against Artemia salina (brine shrimp) and one tumor cell line, namely human Prostate Cancer cell line (PC-3). All the compounds showed low toxicity against brine shrimp with LD50 values much lower than the standard etoposide. Similarly, a much lower toxicity was observed for all the compounds against PC-3 cell line compared to doxorubicin, a standard reference drug used for this study. The molecular docking studies were also carried out to support the experimental results. A good correlation was found between experimental and theoretical results. The compounds of this series are therefore excellent antiglycating agents with no or very little cytotoxicity and represent a new class of antiglycating agents that deserve to be focused on for further research and in vivo studies in the future.
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Evaluation of 4-alkoxychalcones as a new class of antiglycating agents: a combined experimental and docking study

Abstract

A series of 4-alkoxychalcones (1–12) has been evaluated for their in vitro antiglycation activity. Compound 2 (IC50 = 89.07 ± 1.3 μM), compound 3 (IC50 = 266.82 ± 4.6 μM), and compound 5 (IC50 = 285.79 ± 1.9 μM) showed an excellent antiglycation potential better than the standard (rutin, IC50 = 294.50 ± 1.5 μM). Additionally, all the compounds of this series were evaluated for their cytotoxicity against Artemia salina (brine shrimp) and one tumor cell line, namely human Prostate Cancer cell line (PC-3). All the compounds showed low toxicity against brine shrimp with LD50 values much lower than the standard etoposide. Similarly, a much lower toxicity was observed for all the compounds against PC-3 cell line compared to doxorubicin, a standard reference drug used for this study. The molecular docking studies were also carried out to support the experimental results. A good correlation was found between experimental and theoretical results. The compounds of this series are therefore excellent antiglycating agents with no or very little cytotoxicity and represent a new class of antiglycating agents that deserve to be focused on for further research and in vivo studies in the future.